反应详情

355 mg crude N-Hydroxy-4-[6-(4-trifluoromethyl-phenyl)-3,4-dihydro-2H-quinolin-1-yl]-benzamidine were dissolved in 4 ml dichloromethane. 73 μl pyridine and 113 μl phenylchloroformate were added and the mixture stirred at room temperature for ten minutes. The mixture was diluted by the addition of 4 ml acetonitrile and 558 μl 1,8-diazabicyclo[5.4.0]undec-7-ene were added. The mixture was stirred at room temperature for 15 minutes. The mixture was evaporated in vacuo and the resulting crude material was purified by reversed phase HPLC to obtain 209 mg 3-{4-[6-(4-Trifluoromethyl-phenyl)-3,4-dihydro-2H-quinolin-1-yl]-phenyl}-4H-[1,2,4]oxadiazol-5-one.

1. additionwere added
2. stirringThe mixture was stirred at room temperature for 15 minutes
3. customThe mixture was evaporated in vacuo
4. customthe resulting crude material was purified by reversed phase HPLC